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RK-287107
CAS No. 2171386-10-8
RK-287107( —— )
Catalog No. M23984 CAS No. 2171386-10-8
RK-287107 is an effective and specific inhibitor of tankyrase (IC50s: 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 77 | In Stock |
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| 5MG | 67 | In Stock |
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| 10MG | 106 | In Stock |
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| 25MG | 201 | In Stock |
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| 50MG | 277 | In Stock |
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| 100MG | 383 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameRK-287107
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NoteResearch use only, not for human use.
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Brief DescriptionRK-287107 is an effective and specific inhibitor of tankyrase (IC50s: 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively).
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DescriptionRK-287107 is an effective and specific inhibitor of tankyrase (IC50s: 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively).
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In VitroRK-87107 (0.01-10 μM; 12 hours) shows an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli (APC) mutations. The 50% growth inhibition (GI50) value of RK-287107 on COLO-320DM cells is 0.449 μM. RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2. RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells. Cell Proliferation Assay Cell Line:Colorectal cancer COLO-320DM, SW403, RKO, HCC2998, HCT-116, and DLD-1 cells Concentration:0.01, 0.1, 1, 10 μM Incubation Time:12 hours Result:Inhibited the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells. The GI50 value of RK-287107 on COLO-320DM is 0.449 μM. Did not inhibit the growth of APC-wild (β-catenin-independent) colorectal cancer cell lines, including RKO, HCT-116, HCC2998 and DLD-1. Western Blot Analysis Cell Line:COLO-320DM cells Concentration:0.03, 0.1, 0.33, 1, 3, and 10 μM Incubation Time:16 hours Result:Downregulation of active β-catenin was observed
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In VivoRK-287107 (100 and 300 mg/kg; i.p. administration; once per day; 5-days on/ 2-days off schedule for 2 weeks) inhibits tumor growth in a mouse xenograft model. Animal Model:6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM Dosage:100 and 300 mg/kg Administration:Administration i.p.; once per day; 5-days on/ 2-days off schedule for 2 weeks Result:100 and 300 mg/kg resulted in 32.9% and 44.2% TGI, respectively.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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Recptortankyrase 1|tankyrase 2
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Research Area——
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Indication——
Chemical Information
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CAS Number2171386-10-8
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Formula Weight416.46
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Molecular FormulaC22H26F2N4O2
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Purity>98% (HPLC)
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SolubilityDMSO:120 mg/mL (288.14 mM; Need ultrasonic)
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SMILESOCCN(C1)c2cc(F)cc(F)c2C1(CC1)CCN1C(N1)=NC(CCCC2)=C2C1=O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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HIF-1 alpha 556-574
HIF-1 alpha (556-574) is a hypoxia-inducible factor-1 19-mer fragment. HIF-1 functions as master regulator of response to oxygen homeostasis. Hypoxia-induced gene expression is initiated when HIF-1subunit is stabilized in response to a lack of oxygen. This part of HIF-1 binds to the von Hippel-Lindau factor (VHL) an E3 ubiquitin ligase, and the proline 564 is absolutely vital to the binding process.
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RR-src acetate
RR-src acetate is a synthetic peptide derived from the amino acid sequence surrounding the phosphorylation site in pp60src.
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α-Factor Mating Pher...
The alpha factor pheromone arrests yeast in the G1 phase of their cell cycle. Alpha Factor Mating Pheromone induces the expression of mating genes, changes in nuclear architecture, and polarzes growth toward the mating partner.
